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In vitro activity of an oral iminomethoxy aminothiazolyl cephalosporin, R-3746.
- Source :
-
Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 1988 May; Vol. 32 (5), pp. 671-7. - Publication Year :
- 1988
-
Abstract
- The in vitro activity of R-3746, an iminomethoxy aminothiazolyl cephalosporin with a CH2OCH3 moiety at position 3, was compared with those of other antibiotics. R-3746 inhibited the majority of hemolytic streptococci (groups A, B, C, F, and G) and Streptococcus pneumoniae at less than 0.06 micrograms/ml, which was comparable to the activity of amoxicillin, 2- to 8-fold more active than cefixime, and 16- to 64-fold more active than cefaclor and cephalexin. Ninety percent of beta-lactamase-producing Haemophilus influenzae and Neisseria gonorrhoeae were inhibited at a concentration 0.25 micrograms/ml, but it was less active against Branhamella spp. It did not inhibit (MIC, greater than 16 micrograms/ml) enterococci, viridans group streptococci, or methicillin-resistant staphylococci. The MICs of R-3746 for 90% of strains tested for Escherichia coli; Klebsiella pneumoniae; Citrobacter diversus; Proteus mirabilis; and Salmonella, Shigella, and Yersinia spp. were less than or equal to 1 micrograms/ml. It was two- to eightfold less active than cefixime but was markedly superior to cefaclor, cephalexin, amoxicillin-clavulanate, and trimethoprimsulfamethoxazole. R-3746 inhibited 50% of Enterobacter cloacae, Enterobacter aerogenes, Citrobacter freundii, Morganella spp., Providencia spp., Proteus vulgaris, and Serratia marcescens at less than or equal to 8 micrograms/ml. Pseudomonas spp. were resistant. Fifty percent of Clostridium spp. were inhibited by 0.5 micrograms/ml, but MICs for Bacteroides spp. were greater than 128 micrograms/ml. R-3746 was not appreciably hydrolyzed by most chromosomal and plasmid-mediated beta-lactamases.
- Subjects :
- Amoxicillin pharmacology
Amoxicillin-Potassium Clavulanate Combination
Anti-Bacterial Agents pharmacology
Cefaclor pharmacology
Cefixime
Cefotaxime analogs & derivatives
Cefotaxime pharmacology
Cefuroxime pharmacology
Cephalexin pharmacology
Cephalosporins metabolism
Clavulanic Acids pharmacology
Culture Media
Drug Combinations pharmacology
Drug Stability
Gram-Negative Bacteria enzymology
Gram-Positive Bacteria enzymology
Humans
Microbial Sensitivity Tests
Sulfamethoxazole pharmacology
Trimethoprim pharmacology
Trimethoprim, Sulfamethoxazole Drug Combination
beta-Lactamases metabolism
Cefpodoxime
Ceftizoxime analogs & derivatives
Cephalosporins pharmacology
Gram-Negative Bacteria drug effects
Gram-Positive Bacteria drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0066-4804
- Volume :
- 32
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Antimicrobial agents and chemotherapy
- Publication Type :
- Academic Journal
- Accession number :
- 3260766
- Full Text :
- https://doi.org/10.1128/AAC.32.5.671